Transport− Metabolism Interplay

L Salphati - Molecular pharmaceutics, 2009 - ACS Publications
The hypothesis that cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp) played
complementary roles in drug absorption and disposition was first proposed 15 years ago. 1 …

Transporter–enzyme interplay and the hepatic drug clearance: what have we learned so far?

RV Alluri, R Li, MVS Varma - Expert opinion on drug metabolism & …, 2020 - Taylor & Francis
Introduction: Transporters and enzymes play an important role in absorption, distribution,
clearance and elimination of drugs. Areas covered: This review provides an overview of the …

Interplay of drug-metabolizing enzymes and transporters in drug absorption and disposition

S Shi, Y Li - Current drug metabolism, 2014 - ingentaconnect.com
In recent years, the functional interplay between drug-metabolizing enzymes (DMEs) and
drug transporters (DTs) in drug absorption and disposition, as well as the complex drug …

The drug transporter− metabolism alliance: uncovering and defining the interplay

LZ Benet - Molecular pharmaceutics, 2009 - ACS Publications
Two decades ago the importance of transporter− enzyme interplay and its effects on drug
bioavailability and hepatic disposition were first recognized. Here we review the history of …

Transporter-enzyme interactions: implications for predicting drug-drug interactions from in vitro data

LZ Benet, CL Cummins, CY Wu - Current drug metabolism, 2003 - ingentaconnect.com
As discussed in earlier articles, predictions of in vivo drug-drug interactions from in vitro
studies is a subject of high interest with obvious therapeutic as well as economic benefits …

Scientific and regulatory perspectives on metabolizing enzyme− transporter interplay and its role in drug interactions: challenges in predicting drug interactions

L Zhang, Y Zhang, SM Huang - Molecular pharmaceutics, 2009 - ACS Publications
Both metabolizing enzymes and drug transporters play important roles in modulating drug
absorption, distribution, metabolism and elimination. Acting alone or in concert with each …

Functional interactions between P-glycoprotein and CYP3A in drug metabolism

U Christians, V Schmitz, M Haschke - Expert opinion on drug …, 2005 - Taylor & Francis
The interaction between drug-metabolising enzymes and active transporters is an emerging
concept in pharmacokinetics. In the gut mucosa, P-glycoprotein and cytochrome P450 (CYP) …

Impact of hepatic uptake transporters on pharmacokinetics and drug− drug interactions: use of assays and models for decision making in the pharmaceutical industry

MG Soars, PJH Webborn, RJ Riley - Molecular pharmaceutics, 2009 - ACS Publications
The ability to predict hepatic metabolic clearance is a key component in the design and
selection of small molecule drug candidates within the pharmaceutical industry. The …

In vitro and in vivo approaches to characterize transporter-mediated disposition in drug discovery

B Feng, MV Varma, C Costales, H Zhang… - Expert opinion on drug …, 2014 - Taylor & Francis
Introduction: It is becoming increasingly evident that transporters play an important role in
the absorption, distribution and elimination of many drugs. Different approaches have been …

Application of model-based approaches to evaluate hepatic transporter-mediated drug clearance: in vitro, in vivo, and in vitro-in vivo extrapolation

Z Liu, K Liu - Current drug metabolism, 2016 - ingentaconnect.com
Background: Hepatic transporters, including efflux transporters and uptake transporters,
have been recognized to play an important role in the disposition of various drugs. These …